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Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging (2018)
Journal Article
Zamberlan, F., Turyanska, L., Patanè, A., Liu, Z., Williams, H., Fay, M., …Grabowska, A. (in press). Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging. Journal of Materials Chemistry B, 6, https://doi.org/10.1039/c7tb02912h

The short shelf-life of water-soluble quantum dots (QDs) due to colloidal instability represents a major drawback to their exploitation. This work examines the colloidal stability of PbS nanoparticles capped with dihydrolipoic acid–polyethylene glyco... Read More about Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging.

Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group (2017)
Journal Article
Perego, P., Hempel, G., Linder, S., Bradshaw, T. D., Larsen, A. K., Peters, G. J., & Phillips, R. M. (in press). Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group. Cancer Chemotherapy and Pharmacology, https://doi.org/10.1007/s00280-017-3502-7

An increasing number of manuscripts focus on the in vitro evaluation of established and novel anti-tumour agents in experimental models. Whilst the design of such in vitro assays is inherently flexible, some of these studies lack the minimum informat... Read More about Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group.

Development of a series of bis-triazoles as G-quadruplex ligands (2017)
Journal Article
Saleh, M., Laughton, C. A., Bradshaw, T. D., & Moody, C. J. (in press). Development of a series of bis-triazoles as G-quadruplex ligands. RSC Advances, 7, https://doi.org/10.1039/c7ra07257k

Maintenance of telomeres – specialized complexes that protect the ends of chromosomes – is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells. Targeting... Read More about Development of a series of bis-triazoles as G-quadruplex ligands.

In vitro antitumor effects of AHR ligands aminoflavone (AFP 464) and benzothiazole (5F 203) in human renal carcinoma cells (2017)
Journal Article
Luzzani, G. A., Callero, M. A., Kuruppu, A. I., Trapani, V., Flumian, C., Todaro, L., …Loaiza Perez, A. I. (in press). In vitro antitumor effects of AHR ligands aminoflavone (AFP 464) and benzothiazole (5F 203) in human renal carcinoma cells. Journal of Cellular Biochemistry, https://doi.org/10.1002/jcb.26114

We investigated activity and mechanism of action of two AhR ligand antitumor agents, AFP 464 and 5F 203 on human renal cancer cells, specifically examining their effects on cell cycle progression, apoptosis, and migration. TK-10, SN12C, Caki-1, and A... Read More about In vitro antitumor effects of AHR ligands aminoflavone (AFP 464) and benzothiazole (5F 203) in human renal carcinoma cells.

Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1) (2017)
Journal Article
Chung, F. F., Tan, P. F. T. M., Raja, V. J., Tan, B., Lim, K., Kam, T., …Leong, C. (2017). Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1). Scientific Reports, 7(42504), https://doi.org/10.1038/srep42504

Precursor mRNA (pre-mRNA) splicing is catalyzed by a large ribonucleoprotein complex known as the spliceosome. Numerous studies have indicated that aberrant splicing patterns or mutations in spliceosome components, including the splicing factor 3b su... Read More about Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1).

Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors (2017)
Journal Article
Schwehm, C., Kellam, B., Garces, A., Hill, S. J., Kindon, N., Bradshaw, T. D., …Stocks, M. (2017). Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors. Journal of Medicinal Chemistry, 60(4), https://doi.org/10.1021/acs.jmedchem.6b01801

A novel molecular scaffold has been synthesized, and its incorporation into new analogues of biologically active molecules across multiple target classes will be discussed. In these studies, we have shown use of the tricyclic scaffold to synthesize p... Read More about Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors.

Using titanium complexes to defeat cancer: the view from the shoulders of titans (2017)
Journal Article
Cini, M., Bradshaw, T. D., & Woodward, S. (in press). Using titanium complexes to defeat cancer: the view from the shoulders of titans. Chemical Society Reviews, https://doi.org/10.1039/C6CS00860G

When the first titanium complex with anticancer activity was identified in the 1970s, it was attractive, based on the presence of the dichloride unit in TiCl2Cp2 (Cp = ?-C5H5)2, to assume its mode of biological action was closely aligned with cisplat... Read More about Using titanium complexes to defeat cancer: the view from the shoulders of titans.

Cudraflavone C induces tumor-specific apoptosis in colorectal cancer cells through inhibition of the phosphoinositide 3-kinase (PI3K)-AKT pathway (2017)
Journal Article
Castresana, J. S., Soo, H., Chung, F. F., Lim, K., Yap, V. A., Bradshaw, T. D., …Mai, C. (2017). Cudraflavone C induces tumor-specific apoptosis in colorectal cancer cells through inhibition of the phosphoinositide 3-kinase (PI3K)-AKT pathway. PLoS ONE, 12(1), Article e0170551. https://doi.org/10.1371/journal.pone.0170551

Cudraflavone C (Cud C) is a naturally-occurring flavonol with reported anti-proliferative activities. However, the mechanisms by which Cud C induced cytotoxicity have yet to be fully elucidated. Here, we investigated the effects of Cud C on cell prol... Read More about Cudraflavone C induces tumor-specific apoptosis in colorectal cancer cells through inhibition of the phosphoinositide 3-kinase (PI3K)-AKT pathway.

Antitumor imidazo[5,1-d]-1,2,3,5-tetrazines: compounds modified at the 3-position overcome resistance in human glioblastoma cell lines (2016)
Journal Article
Cousin, D., Zhang, J., Hummersone, M. G., Matthews, C. S., Frigerio, M., Bradshaw, T., & Stevens, M. F. (2016). Antitumor imidazo[5,1-d]-1,2,3,5-tetrazines: compounds modified at the 3-position overcome resistance in human glioblastoma cell lines. MedChemComm, 7(12), 2332-2343. doi:10.1039/c6md00384b

Synthetic routes to 3-substituted imidazo[5,1-d]-1,2,3,5-tetrazines structurally related to temozolomide were explored. Interaction of 4-diazoimidazole-5-carboxamide with an isocyanate afforded high product yields when the isocyanate was available in... Read More about Antitumor imidazo[5,1-d]-1,2,3,5-tetrazines: compounds modified at the 3-position overcome resistance in human glioblastoma cell lines.

In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B (2015)
Journal Article
Qazzaz, M. E., Raja, V. J., Lim, K., Kam, T., Lee, J. B., Gershkovich, P., & Bradshaw, T. D. (2016). In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B. Cancer Letters, 370(2), https://doi.org/10.1016/j.canlet.2015.10.013

Natural products play a pivotal role in medicine especially in the cancer arena. Many drugs that are currently used in cancer chemotherapy originated from or were inspired by nature. Jerantinine B (JB) is one of seven novel Aspidosperma indole alkalo... Read More about In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B.

Asymmetric pentafulvene carbometalation-access to enantiopure titanocene dichlorides of biological relevance (2015)
Journal Article
Cini, M., Bradshaw, T. D., Woodward, S., & Lewis, W. (2015). Asymmetric pentafulvene carbometalation-access to enantiopure titanocene dichlorides of biological relevance. Angewandte Chemie International Edition, 54(47), https://doi.org/10.1002/anie.201508034

Unprecedented asymmetric copper-catalyzed addition of ZnEt2 (ZnBu2) to the exocyclic C[DOUBLE BOND]C bond of pentafulvenes C5H4([DOUBLE BOND]CHAr) (Ar=2-MeOPh and related species) results in enantiomerically enriched (up to 93:7 e.r.) cyclopentadieny... Read More about Asymmetric pentafulvene carbometalation-access to enantiopure titanocene dichlorides of biological relevance.

Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery (2015)
Journal Article
Stone, E. L., Citossi, F., Singh, R., Kaur, B., Gaskell, M., Farmer, P. B., …Bradshaw, T. D. (2015). Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery. Bioorganic and Medicinal Chemistry, 23(21), 6891-6899. https://doi.org/10.1016/j.bmc.2015.09.052

Potent, selective antitumour AhR ligands 5F 203 and GW 610 are bioactivated by CYPs 1A1 and 2W1. Herein we reason that DNA adducts’ generation resulting in lethal DNA double strand breaks (DSBs) underlies benzothiazoles’ activity. Treatment of sensit... Read More about Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery.

Gelation properties of self-assembling N-acyl modified cytidine derivatives (2014)
Journal Article
Skilling, K. J., Ndungu, A., Kellam, B., Ashford, M., Bradshaw, T. D., & Marlow, M. (in press). Gelation properties of self-assembling N-acyl modified cytidine derivatives. Journal of Materials Chemistry B, 2(47), https://doi.org/10.1039/C4TB01375A

In this study we report the synthesis of new cytidine derived gelators possessing acyl chains of different lengths. These low molecular weight gelators were shown to form self-supporting gels at 0.5 % (w/v) in binary systems of aqueous miscible polar... Read More about Gelation properties of self-assembling N-acyl modified cytidine derivatives.

In vitro antitumor mechanism of (E)-N-(2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)pyridin-3-yl)methanesulfonamide (2014)
Journal Article
Lu, T., Laughton, C., Wang, S., & Bradshaw, T. (2015). In vitro antitumor mechanism of (E)-N-(2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)pyridin-3-yl)methanesulfonamide. Molecular Pharmacology, 87(1), 18-30. doi:10.1124/mol.114.093245

ON01910.Na [sodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate; Rigosertib, Estybon], a styryl benzylsulfone, is a phase III stage anticancer agent. This non-ATP competitive kinase inhibitor has multitargeted activi... Read More about In vitro antitumor mechanism of (E)-N-(2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)pyridin-3-yl)methanesulfonamide.

Overcoming multiple drug resistance mechanisms in medulloblastoma (2014)
Journal Article
Othman, R., Coyle, B., Kimishi, I., Bradshaw, T. D., Storer, L., Korshunov, A., …Kerr, I. D. (2014). Overcoming multiple drug resistance mechanisms in medulloblastoma. Acta Neuropathologica Communications, 2(1), Article 57. https://doi.org/10.1186/2051-5960-2-57

© 2014 Othman et al.; licensee BioMed Central Ltd. Introduction: Medulloblastoma (MB) is the most common malignant paediatric brain tumour. Recurrence and progression of disease occurs in 15-20% of standard risk and 30-40% of high risk patients. We a... Read More about Overcoming multiple drug resistance mechanisms in medulloblastoma.

Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73 (2014)
Journal Article
Lam, F., Abbas, A. Y., Shao, H., Teo, T., Adams, J., Li, P., …Wang, S. (2014). Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73. Oncotarget, 5(17), 7691–7704. https://doi.org/10.18632/oncotarget.2296

Dysregulation of cellular transcription and translation is a fundamental hallmark of cancer. As CDK9 and Mnks play pivotal roles in the regulation of RNA transcription and protein synthesis, respectively, they are important targets for drug developme... Read More about Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73.

A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine (2013)
Journal Article
Walsby, E., Pratt, G., Shao, H., Abbas, A. Y., Fischer, P., Bradshaw, T. D., …Pepper, C. (2013). A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine. Oncotarget, 5, 375-385

Cdk9 is a key elongation factor for RNA transcription and functions by phosphorylating the C-terminal domain of RNA polymerase II. Here we present direct evidence that cdk9 is important for cancer cell survival and describe the characterization of th... Read More about A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine.

Apoferritin-encapsulated PbS quantum dots significantly inhibit growth of colorectal carcinoma cells (2013)
Journal Article
Bradshaw, T. D., Junor, M., Patanè, A., Clarke, P., Thomas, N. R., Li, M., …Turyanska, L. (2013). Apoferritin-encapsulated PbS quantum dots significantly inhibit growth of colorectal carcinoma cells. Journal of Materials Chemistry B, 45, 6254-6260. https://doi.org/10.1039/c3tb21197e

Colorectal carcinoma (CRC) is the 3rd most common cancer worldwide, thus development of novel therapeutic strategies is imperative. Herein potent, selective dose-dependent antitumor activity of horse spleen apoferritin encapsulated PbS quantum dots (... Read More about Apoferritin-encapsulated PbS quantum dots significantly inhibit growth of colorectal carcinoma cells.

Paramagnetic, near-infrared fluorescent Mn-doped PbS colloidal nanocrystals (2013)
Journal Article
Turyanska, L., Moro, F., Knott, A. N., Fay, M. W., Bradshaw, T. D., & Patanè, A. (2013). Paramagnetic, near-infrared fluorescent Mn-doped PbS colloidal nanocrystals. Particle and Particle Systems Characterization, 30(11), https://doi.org/10.1002/ppsc.201300184

Mn-doped PbS colloidal nanocrystals in aqueous solution are paramagnetic and optically active in the technologically important biological window between 1.2 and 0.8 ?m. Cytoxicity studies show that exposure of human cell lines to the nanoparticles at... Read More about Paramagnetic, near-infrared fluorescent Mn-doped PbS colloidal nanocrystals.